Design, Bioactivity and structure-activity of 3-Arylpropionate Derivatives as Potential High-Efficient Acaricides against Psoroptes Cuniculi.

ABSTRACT: A series of 3-aryl propionic esters and their analogues were designed and evaluated for acaricidal activity in vitro against Psoroptes cuniculi, a mange mite. The structure-activity relationship (SAR) was also discussed. The results showed that 6 compounds possessed the excellent activity (LC₅₀ = 0.17-0.24 mM, LT₅₀ = 1.5-2.9 h), superior to ivermectin (LC₅₀ = 0.28 mM, LT₅₀ = 8.9 h) (P < 0.05), a standard drug. Furthermore, 7 compounds showed the good activity (LC₅₀ = 0.25-0.37 mM, LT₅₀ < 3.9 h), slightly lower or close to that of ivermectin. One compound displayed super-fast acaricidal property, far superior to ivermectin. SAR analysis found that the ester group is vital for the activity and the small steric hindrance adjace

SUBMITTER: Chen D 

PROVIDER: S-EPMC5788918 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature